The purpose of this study is to assess how well laroprovstat and ezetimibe combined in a single tablet to be taken by mouth works and what the body does to the drug (pharmacokinetics) compared with laroprovstat and ezetimibe individual tablets to be taken by mouth (relative bioavailability) as well as to see if there is any effect of eating compared to fasting (food effect) in healthy adults.
Healthy male and female participants aged 18 to 55 years at the time of signing consent.
All females must have a negative pregnancy test at the Screening Visit and on admission to the study site.
Females of childbearing potential must not be lactating and if heterosexually active must agree to use an approved method of highly effective contraception.
Have a Body mass index (BMI) between 18 and 30 kg/m2 inclusive and weigh at least 50 kg.
History of any clinically important disease or disorder.
History or presence of gastrointestinal, hepatic, or renal disease or any other condition known to interfere with absorption, distribution, metabolism, or excretion of drugs.
History of severe allergy/hypersensitivity or ongoing clinically important allergy/hypersensitivity to drugs with a similar chemical structure or class to laroprovstat or ezetimibe.
Treatment with any lipid lowering therapy or laroprovstat within the 3 months prior to the Screening Visit.
Crossover
Laroprovstat/ezetimibe FCDP
DrugLaroprovstat/ezetimibe will be administered orally.
Laroprovstat STP
DrugLaroprovstat will be administered orally.
Ezetimibe STP
DrugEzetimibe will be administered orally.
Laroprovstat/ezetimibe FCDP-slow variant
DrugLaroprovstat/ezetimibe slow variant will be administered orally
Area under concentration-time curve from time 0 to infinity (AUCinf)
To evaluate the relative bioavailability between the FCDPs and the STPs of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe.
Area under concentration-curve from time 0 to the last quantifiable concentration (AUClast)
To evaluate the relative bioavailability between the FCDPs and the STPs of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe.
Maximum observed drug concentration (Cmax)
To evaluate the relative bioavailability between the FCDPs and the STPs of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe.
Plasma Time to reach maximum observed concentration (tmax)
To examine the pharmacokinetic (PK) profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.
Terminal elimination half-life (t½λz)
To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.
Apparent total body clearance (CL/F)
To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.
Apparent volume of distribution based on the terminal phase (Vz/F)
To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.
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